Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XJKXB
ADC Name
Trastuzumab-C239I-SG3400
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
1.71
Structure
Antibody Name
Engineered trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
SG3200
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Mal-PEG8-Val-Ala-PABC
  Linker Info 
Conjugate Type
Coupling of cysteine sulfhydryl groups in antibodies with maleimide.
Combination Type
SG3400
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 40.5
%
Breast cancer cells
Breast cancer
Tumor Growth Inhibition value (TGI) 
≈ 48
%
Gastric cancer cells
Gastric cancer
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
10.7
ng/mL
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
20.9
ng/mL
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
23.3
ng/mL
MDA-MB-231 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 50
ng/mL
MCF-7 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 250
ng/mL
JIMT-1 cells
Breast ductal carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 40.50% (Day 50) Negative expression (HER2-)
Method Description
The antitumor activity of trastuzumab-C239i-SG3400 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model Breast cancer CDX model
In Vitro Model Breast cancer Breast cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 48.00% (Day 50) Low HER2 expression (HER2+)
Method Description
The antitumor activity of trastuzumab-C239i-SG3400 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model Gastric cancer CDX model
In Vitro Model Gastric cancer Gastric cancer cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 10.70 ng/mL Low HER2 expression (HER2+)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 20.90 ng/mL Low HER2 expression (HER2+)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 23.30 ng/mL Low HER2 expression (HER2+)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50.00 ng/mL Negative expression (HER2-)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 250.00 ng/mL Negative expression (HER2-)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
References
Ref 1 Synthesis and evaluation of pyrrolobenzodiazepine dimer antibody-drug conjugates with dual -glucuronide and dipeptide triggers. Eur J Med Chem. 2019 Oct 1;179:591-607.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.